WO2021048613A3 - Penam derivatives for treating bacterial infections - Google Patents

Penam derivatives for treating bacterial infections Download PDF

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Publication number
WO2021048613A3
WO2021048613A3 PCT/IB2020/000686 IB2020000686W WO2021048613A3 WO 2021048613 A3 WO2021048613 A3 WO 2021048613A3 IB 2020000686 W IB2020000686 W IB 2020000686W WO 2021048613 A3 WO2021048613 A3 WO 2021048613A3
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WO
WIPO (PCT)
Prior art keywords
bacterial infections
treating bacterial
penam derivatives
penam
antibacterial agents
Prior art date
Application number
PCT/IB2020/000686
Other languages
French (fr)
Other versions
WO2021048613A2 (en
WO2021048613A8 (en
Inventor
Jun Ding
Zhijun Zhuang
Ying Yuan
Yu Liu
Shijie He
Qian Zhang
Zhenku MA
Dawei Wan
Huibing Ai
Huan Wang
Original Assignee
Tennor Therapeutics Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tennor Therapeutics Limited filed Critical Tennor Therapeutics Limited
Priority to EP20862212.6A priority Critical patent/EP4028404A4/en
Priority to JP2022516222A priority patent/JP2022548067A/en
Priority to CN202080062847.6A priority patent/CN114423766B/en
Publication of WO2021048613A2 publication Critical patent/WO2021048613A2/en
Publication of WO2021048613A3 publication Critical patent/WO2021048613A3/en
Publication of WO2021048613A8 publication Critical patent/WO2021048613A8/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D499/87—Compounds being unsubstituted in position 3 or with substituents other than only two methyl radicals attached in position 3, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C07D519/06—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 containing at least one condensed beta-lactam ring system, provided for by groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00, e.g. a penem or a cepham system

Abstract

Novel iron chelating group conjugated penam derivatives described herein show antibacterial activity, and could be used as antibacterial agents or beta-lactamase inhibitors (BLIs) which are of value for application in combination with other antibacterial agents. (Formula I)
PCT/IB2020/000686 2019-09-11 2020-08-25 Penam derivatives for treating bacterial infections WO2021048613A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP20862212.6A EP4028404A4 (en) 2019-09-11 2020-08-25 Penam derivatives for treating bacterial infections
JP2022516222A JP2022548067A (en) 2019-09-11 2020-08-25 Penam derivatives for treating bacterial infections
CN202080062847.6A CN114423766B (en) 2019-09-11 2020-08-25 Pentane derivatives for the treatment of bacterial infections

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962898598P 2019-09-11 2019-09-11
US62/898,598 2019-09-11

Publications (3)

Publication Number Publication Date
WO2021048613A2 WO2021048613A2 (en) 2021-03-18
WO2021048613A3 true WO2021048613A3 (en) 2021-05-20
WO2021048613A8 WO2021048613A8 (en) 2022-05-12

Family

ID=74850748

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2020/000686 WO2021048613A2 (en) 2019-09-11 2020-08-25 Penam derivatives for treating bacterial infections

Country Status (4)

Country Link
US (1) US11040987B2 (en)
EP (1) EP4028404A4 (en)
JP (1) JP2022548067A (en)
WO (1) WO2021048613A2 (en)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997006172A1 (en) * 1995-08-04 1997-02-20 Synphar Laboratories, Inc. Novel penam sulfones as beta-lactamase inhibitors
WO2002022613A1 (en) * 2000-09-14 2002-03-21 Pantherix Limited 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents
US20040132707A1 (en) * 2001-03-01 2004-07-08 Gruenenthal Gmbh Catecholate beta-lactam conjugates, method for producing the same and the use thereof
WO2012070071A1 (en) * 2010-11-25 2012-05-31 Orchid Research Laboratories Ltd Compounds and their use
WO2018014823A1 (en) * 2016-07-21 2018-01-25 中国科学院上海药物研究所 Monocyclic β-lactam-iron carrier conjugate, and manufacturing method and application thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1239392A (en) * 1983-10-13 1988-07-19 Shigeru Yamabe Penicillin derivatives and process for preparing the same
US4861768A (en) * 1986-02-27 1989-08-29 Taiho Pharmaceutical Company, Limited 2 β-substituted thiomethylpenicillin derivatives and their preparation and use
US8299051B2 (en) 2008-05-13 2012-10-30 Southern Methodist University Beta-lactamase inhibitory compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997006172A1 (en) * 1995-08-04 1997-02-20 Synphar Laboratories, Inc. Novel penam sulfones as beta-lactamase inhibitors
WO2002022613A1 (en) * 2000-09-14 2002-03-21 Pantherix Limited 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents
US20040132707A1 (en) * 2001-03-01 2004-07-08 Gruenenthal Gmbh Catecholate beta-lactam conjugates, method for producing the same and the use thereof
WO2012070071A1 (en) * 2010-11-25 2012-05-31 Orchid Research Laboratories Ltd Compounds and their use
WO2018014823A1 (en) * 2016-07-21 2018-01-25 中国科学院上海药物研究所 Monocyclic β-lactam-iron carrier conjugate, and manufacturing method and application thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BEHARRY, Z. CHEN, H. GADHACHANDA, V.R. BUYNAK, J.D. PALZKILL, T.: "Evaluation of penicillin-based inhibitors of the class A and B @b-lactamases from Bacillus anthracis", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 313, no. 3, 16 January 2004 (2004-01-16), Amsterdam NL, pages 541 - 545, XP004481591, ISSN: 0006-291X, DOI: 10.1016/j.bbrc.2003.11.158 *
PATTANAIK P.ET AL.: "Strategic Design of an Effective β-Lactamase Inhibitor LN-1-255， A 6-ALKYLIDENE-2'-SUBSTITUTED PENICILLIN SULFONE；", THE JOURNAL OF BIOLOGICAL CHEMISTRY；, vol. 284, no. 2, 9 January 2009 (2009-01-09), XP055788965 *

Also Published As

Publication number Publication date
CN114423766A (en) 2022-04-29
WO2021048613A2 (en) 2021-03-18
WO2021048613A8 (en) 2022-05-12
EP4028404A2 (en) 2022-07-20
US11040987B2 (en) 2021-06-22
JP2022548067A (en) 2022-11-16
EP4028404A4 (en) 2023-07-26
US20210070774A1 (en) 2021-03-11

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